Mutant IDH1 inhibitor

Name: Mutant IDH1 inhibitor
Brand: MedChemExpress
SKU: HY-13972
Rating: 5.0 (3 reviews)

Cat. No.: HY-13972 Purity: 99.40%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC₅₀ of < 72 nM.

For research use only. We do not sell to patients.

Mutant IDH1 inhibitor Chemical Structure

CAS No. : 1429180-08-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 175	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 175	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 690	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE Mutant IDH1 inhibitor

: Mutant IDH1 inhibitor purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758. [Abstract]; Represented western blot of an isothermal dose-response at melting temperature of 59°C demonstrating cellular mIDH1 enzyme thermal stabilization with mIDH1 inhibitors.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

View All Isoforms

IDH1 IDH2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC₅₀ of < 72 nM.

IC₅₀ & Target

IC50: < 72 nM (mutant IDH1 R132H)

In Vitro

Mutant IDH1 inhibitor is a potent IDH1 R132H inhibitor, and used for the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

466.58

Formula

C₂₅H₃₄N₆O₃

CAS No.

1429180-08-4

Appearance

Solid

Color

White to light yellow

SMILES

CC(C)[C@@H](COC1=O)N1C2=NC(N[C@@H](C)C3=CC=C(CN4CCN(C(C)=O)CC4)C=C3)=NC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 34 mg/mL (72.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1433 mL	10.7163 mL	21.4326 mL
5 mM	0.4287 mL	2.1433 mL	4.2865 mL
10 mM	0.2143 mL	1.0716 mL	2.1433 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.40%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (251 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. 3-Pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH and their preparation. Patent WO 2013046136 A1 20130404

Cell Assay
^[1]

Day 1: cells are seeded in 384-well plates in triplicates for both the cell proliferation and 2HG assay, and incubated at 37°C, 95% Rh, 5% CO₂ overnight. Day 2: compounds are serially diluted 1 :3 (10 point dilution from 10 mM solutions in DMSO) and delivered to the cell assay plates via acoustic dispenser, with final concentration ranging from 30 μM to 1.5 nM. The plates are returned to the incubator after treatment and incubated for 48 hours. Day 4 Proliferation assay: CTG is added to the assay plates and luminescence signal is read on the plate reader. Day 4 2HG assay : Extraction sample preparation consisted of aspirating all media from the assay plates, adding 70 μL of 90% methanol in water, dry ice incubation for 15 minutes, centrifuging at 2000 rpm for 30 min to ensure all particulates have settled, and transferring 30 μL of the supernatant into LC-MS ready plates. LC-MS analysis follows.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. 3-Pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH and their preparation. Patent WO 2013046136 A1 20130404

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1433 mL	10.7163 mL	21.4326 mL	53.5814 mL
	5 mM	0.4287 mL	2.1433 mL	4.2865 mL	10.7163 mL
	10 mM	0.2143 mL	1.0716 mL	2.1433 mL	5.3581 mL
	15 mM	0.1429 mL	0.7144 mL	1.4288 mL	3.5721 mL
	20 mM	0.1072 mL	0.5358 mL	1.0716 mL	2.6791 mL
	25 mM	0.0857 mL	0.4287 mL	0.8573 mL	2.1433 mL
	30 mM	0.0714 mL	0.3572 mL	0.7144 mL	1.7860 mL
	40 mM	0.0536 mL	0.2679 mL	0.5358 mL	1.3395 mL
	50 mM	0.0429 mL	0.2143 mL	0.4287 mL	1.0716 mL
	60 mM	0.0357 mL	0.1786 mL	0.3572 mL	0.8930 mL